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ES2850278B2 - COMPLEJO DE ETINIL ESTRADIOL-ß-CICLODEXTRINA Y PROCEDIMIENTO PARA SU PREPARACION - Google Patents

COMPLEJO DE ETINIL ESTRADIOL-ß-CICLODEXTRINA Y PROCEDIMIENTO PARA SU PREPARACION Download PDF

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Publication number
ES2850278B2
ES2850278B2 ES202190031A ES202190031A ES2850278B2 ES 2850278 B2 ES2850278 B2 ES 2850278B2 ES 202190031 A ES202190031 A ES 202190031A ES 202190031 A ES202190031 A ES 202190031A ES 2850278 B2 ES2850278 B2 ES 2850278B2
Authority
ES
Spain
Prior art keywords
ethinyl estradiol
cyclodextrin
amorphous
complex
tetrahydrofolic acid
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
ES202190031A
Other languages
English (en)
Spanish (es)
Other versions
ES2850278R1 (es
ES2850278A2 (es
Inventor
Ortega María Dolores Moya
Andreza Maria Ribeiro
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Laboratorios Leon Farma SA
Original Assignee
Laboratorios Leon Farma SA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Laboratorios Leon Farma SA filed Critical Laboratorios Leon Farma SA
Publication of ES2850278A2 publication Critical patent/ES2850278A2/es
Publication of ES2850278R1 publication Critical patent/ES2850278R1/es
Application granted granted Critical
Publication of ES2850278B2 publication Critical patent/ES2850278B2/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • A61K9/1694Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40Cyclodextrins; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6949Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
    • A61K47/6951Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Reproductive Health (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
ES202190031A 2018-12-13 2019-12-11 COMPLEJO DE ETINIL ESTRADIOL-ß-CICLODEXTRINA Y PROCEDIMIENTO PARA SU PREPARACION Active ES2850278B2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18382921.7A EP3666260A1 (fr) 2018-12-13 2018-12-13 Complexe d'éthinyl estradiol-beta-cyclodextrine et son procédé de preparation
PCT/EP2019/084591 WO2020120548A1 (fr) 2018-12-13 2019-12-11 COMPLEXE D'ÉTHINYLESTRADIOL-β-CYCLODEXTRINE ET SON PROCÉDÉ DE PRÉPARATION

Publications (3)

Publication Number Publication Date
ES2850278A2 ES2850278A2 (es) 2021-08-26
ES2850278R1 ES2850278R1 (es) 2022-12-02
ES2850278B2 true ES2850278B2 (es) 2023-09-15

Family

ID=65003157

Family Applications (1)

Application Number Title Priority Date Filing Date
ES202190031A Active ES2850278B2 (es) 2018-12-13 2019-12-11 COMPLEJO DE ETINIL ESTRADIOL-ß-CICLODEXTRINA Y PROCEDIMIENTO PARA SU PREPARACION

Country Status (5)

Country Link
US (1) US12318395B2 (fr)
EP (1) EP3666260A1 (fr)
JP (1) JP7499252B2 (fr)
ES (1) ES2850278B2 (fr)
WO (1) WO2020120548A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12318395B2 (en) 2018-12-13 2025-06-03 Laboratorios Leon Farma, S.A. Ethinyl estradiol-β-cyclodextrin complex and process for preparing thereof

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114225050B (zh) * 2022-01-29 2022-12-13 国家卫生健康委科学技术研究所 炔雌醇环糊精复合物的制备及应用
CN116617157B (zh) * 2023-05-25 2025-02-18 国家卫生健康委科学技术研究所 一种制备pH响应性炔雌醇复合水凝胶的方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4727064A (en) * 1984-04-25 1988-02-23 The United States Of America As Represented By The Department Of Health And Human Services Pharmaceutical preparations containing cyclodextrin derivatives
DE4426709A1 (de) 1994-07-20 1996-01-25 Schering Ag Steroidale Sexualhormone enthaltende feste Arzneiformen
IT1304190B1 (it) 1998-12-18 2001-03-08 Euphar Group Srl Clatrati di deidroepiandrosterone e relative composizionifarmaceutiche
CH693905A5 (de) 1999-04-15 2004-04-15 Eprova Ag Stabile kristalline Salze von 5-Methyltetrahydrofolsäure.
EP1216713A1 (fr) * 2000-12-20 2002-06-26 Schering Aktiengesellschaft Compositions de complexes de estrogen-cyclodextrine
WO2014056035A1 (fr) 2012-10-10 2014-04-17 The University Of Queensland Encapsulation de gaz dans des cyclodextrines
EP2781214A1 (fr) 2013-03-22 2014-09-24 Chemo Research, S.L. Formulation de calcium amorphe L-5-méthyltétrahydrofolate (L-5-MTHF-Ca)
WO2016097025A1 (fr) 2014-12-19 2016-06-23 Synthon B.V. Composition pharmaceutique comprenant de la lénalidomide amorphe
EP3666260A1 (fr) 2018-12-13 2020-06-17 Laboratorios Leon Farma SA Complexe d'éthinyl estradiol-beta-cyclodextrine et son procédé de preparation

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12318395B2 (en) 2018-12-13 2025-06-03 Laboratorios Leon Farma, S.A. Ethinyl estradiol-β-cyclodextrin complex and process for preparing thereof

Also Published As

Publication number Publication date
EP3666260A1 (fr) 2020-06-17
US20220040200A1 (en) 2022-02-10
ES2850278R1 (es) 2022-12-02
JP7499252B2 (ja) 2024-06-13
WO2020120548A1 (fr) 2020-06-18
ES2850278A2 (es) 2021-08-26
JP2022513237A (ja) 2022-02-07
US12318395B2 (en) 2025-06-03

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